1. Metabolic Enzyme/Protease
  2. Cytochrome P450
  3. Anthraflavic acid

Anthraflavic acid  (Synonyms: アントラフラビン酸)

製品番号: HY-W006230 純度: 99.51%
COA 取扱説明書 Technical Support

Anthraflavic acid specifically inhibits the activity of cytochrome P-448 without affecting phenobarbital-induced cytochrome P-450 or NADPH-dependent cytochrome c reduction. Anthraflavic acid inhibits cytosolic metabolic pathways, blocks the microsomal and cytosolic activation of IQ, and reduces the metabolic activation level of Glu-P-I. Anthraflavic acid may exert anticancer activity by inhibiting the metabolic activation of chemical carcinogens. Anthraflavic acid is applicable to cancer-related research.

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Anthraflavic acid

Anthraflavic acid 構造式

CAS 番号 : 84-60-6

容量 価格(税別) 在庫状況 数量
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
USD 27 在庫あり
Solution
10 mM * 1 mL in DMSO USD 27 在庫あり
Solid
500 mg $25 在庫あり
1 g $40 在庫あり
5 g $100 在庫あり
10 g $140 在庫あり
25 g $225 在庫あり
50 g $315 在庫あり
100 g $440 在庫あり
> 100 g   お問い合わせ  

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製品説明

Anthraflavic acid specifically inhibits the activity of cytochrome P-448 without affecting phenobarbital-induced cytochrome P-450 or NADPH-dependent cytochrome c reduction. Anthraflavic acid inhibits cytosolic metabolic pathways, blocks the microsomal and cytosolic activation of IQ, and reduces the metabolic activation level of Glu-P-I. Anthraflavic acid may exert anticancer activity by inhibiting the metabolic activation of chemical carcinogens. Anthraflavic acid is applicable to cancer-related research[1][2][3].

Cellular Effect
Cell Line Type Value Description References
HEK293 IC50
3.6 μM
Compound: Anthraflavic acid
Inhibition of human recombinant UGT1A1 expressed in HEK293 cells assessed as reduction in bilirubin glucuronidation by LC-MS/MS method
Inhibition of human recombinant UGT1A1 expressed in HEK293 cells assessed as reduction in bilirubin glucuronidation by LC-MS/MS method
[PMID: 21030469]
HEK293 IC50
4 μM
Compound: Anthraflavic acid
Inhibition of human recombinant UGT1A1 expressed in HEK293 cells assessed as reduction in estradiol 3-glucuronidation by LC-MS/MS method
Inhibition of human recombinant UGT1A1 expressed in HEK293 cells assessed as reduction in estradiol 3-glucuronidation by LC-MS/MS method
[PMID: 21030469]
体外実験

Anthraflavic acid (5×10−7-5×10−5 M; 20 min) potently inhibits S9-mediated mutagenicity of IQ in Salmonella typhimurium strain TA98 in a concentration-dependent manner, with complete inhibition observed at 5×10−5 M[1].
Anthraflavic acid (1×10−7-5×10−5 M; 20 min post-microsomal reaction termination) inhibits cytosol-mediated potentiation of microsome-generated IQ mutagenicity in Salmonella typhimurium strain TA98, with a pronounced effect at 5×10−5 M[1].
Anthraflavic acid (5×10−7-5×10−5 M) potently and concentration-dependently reduces cytochrome P-448-dependent Glu-P-1 mutagenicity in the Ames test with Salmonella typhimurium strain TA 98 and an Arochlor-1254-induced rat hepatic S9 activation system, and shows no mutagenic activity itself[2].
Anthraflavic acid (5×10−7-5×10−5 M) does not inhibit NADPH-dependent cytochrome c reductase activity in Arochlor-1254-induced rat hepatic microsomes, even at concentrations up to 5×10−5 M, showing it does not interfere with electron flow to cytochrome P-450[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

体内実験

Anthraflavic acid (100 mg/kg; i.p.; daily; 5 days) is a specific inducer of rat hepatic cytochrome P-450 I proteins, significantly increasing activities of ethoxycoumarin and ethoxyresorufin O-deethylases and enhancing the metabolic activation of the carcinogens Glu-P-1 and IQ to mutagenic intermediates[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Wistar (male, 150-180 g)[3]
Dosage: 100 mg/kg
Administration: i.p.; daily; 5 days
Result: Showed no significant effect on total cytochrome P-450 levels, NADPH-cytochrome c reductase activity, cytosolic protein concentration, microsomal protein concentration, or cytosolic glutathione S-transferase activity.
Increased hepatic microsomal ethoxycoumarin O-deethylase activity to 86.6 pmol/min/mg protein and 164.7 pmol/min/nmol P-450.
Increased hepatic microsomal ethoxyresorufin O-deethylase activity to 0.314 nmol/min/mg protein and 0.59 nmol/min/nmol P-450.
Induced cytochrome P-450 I A1 and P-450 I A2 apoproteins, with no change in P-450 II B1 levels.
分子量

240.21

分子式

C14H8O4

CAS 番号
Appearance

Solid

Color

Yellow to green

SMILES

O=C1C2=C(C=C(O)C=C2)C(C3=CC=C(O)C=C13)=O

輸送条件

Room temperature in continental US; may vary elsewhere.

保管条件

4°C, stored under nitrogen

*In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)

溶剤 & 溶解度
体外: 

DMSO : 16.67 mg/mL (69.40 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 4.1630 mL 20.8151 mL 41.6302 mL
5 mM 0.8326 mL 4.1630 mL 8.3260 mL
10 mM 0.4163 mL 2.0815 mL 4.1630 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
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Concentration
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Volume
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Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

一般には略語で表示されます:C1V1 = C2V2

濃度 (開始)

C1

×
体積 (開始)

V1

=
濃度 (終了)

C2

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体積 (終了)

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体内:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: 1.67 mg/mL (6.95 mM); Suspended solution; Need ultrasonic

    This protocol yields a suspended solution of 1.67 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (16.7 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).

*In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
純度とドキュメンテーション

純度: 99.51%

参考文献

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 4.1630 mL 20.8151 mL 41.6302 mL 104.0756 mL
5 mM 0.8326 mL 4.1630 mL 8.3260 mL 20.8151 mL
10 mM 0.4163 mL 2.0815 mL 4.1630 mL 10.4076 mL
15 mM 0.2775 mL 1.3877 mL 2.7753 mL 6.9384 mL
20 mM 0.2082 mL 1.0408 mL 2.0815 mL 5.2038 mL
25 mM 0.1665 mL 0.8326 mL 1.6652 mL 4.1630 mL
30 mM 0.1388 mL 0.6938 mL 1.3877 mL 3.4692 mL
40 mM 0.1041 mL 0.5204 mL 1.0408 mL 2.6019 mL
50 mM 0.0833 mL 0.4163 mL 0.8326 mL 2.0815 mL
60 mM 0.0694 mL 0.3469 mL 0.6938 mL 1.7346 mL
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  • Molarity Calculator

  • Dilution Calculator

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

質量   濃度   体積   分子量 *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

一般には略語で表示されます:C1V1 = C2V2

濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
× = ×
C1   V1   C2   V2
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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製品名:
Anthraflavic acid
製品番号:
HY-W006230
数量:
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